BR112013006594B1 - Composto ciclopropano antagonista de receptor da orexina e composição farmacêutica - Google Patents

Composto ciclopropano antagonista de receptor da orexina e composição farmacêutica Download PDF

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Publication number
BR112013006594B1
BR112013006594B1 BR112013006594-0A BR112013006594A BR112013006594B1 BR 112013006594 B1 BR112013006594 B1 BR 112013006594B1 BR 112013006594 A BR112013006594 A BR 112013006594A BR 112013006594 B1 BR112013006594 B1 BR 112013006594B1
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Brazil
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group
compound
methyl
oxy
solution
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BR112013006594-0A
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English (en)
Portuguese (pt)
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BR112013006594A2 (pt
Inventor
Taro Terauchi
Ayumi Takemura
Takashi Doko
Yu Yoshida
Toshiaki Tanaka
Keiichi Sorimachi
Yoshimitsu Naoe
Carsten Beuckmann
Yuji Kazuta
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Eisai R&D Management Co., Ltd
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Publication of BR112013006594A2 publication Critical patent/BR112013006594A2/pt
Publication of BR112013006594B1 publication Critical patent/BR112013006594B1/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Anesthesiology (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pulmonology (AREA)
  • Nutrition Science (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
BR112013006594-0A 2010-09-22 2011-09-20 Composto ciclopropano antagonista de receptor da orexina e composição farmacêutica BR112013006594B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US38534210P 2010-09-22 2010-09-22
US61/385,342 2010-09-22
JP2010211629 2010-09-22
JP2010-211629 2010-09-22
PCT/JP2011/071325 WO2012039371A1 (ja) 2010-09-22 2011-09-20 シクロプロパン化合物

Publications (2)

Publication Number Publication Date
BR112013006594A2 BR112013006594A2 (pt) 2016-06-21
BR112013006594B1 true BR112013006594B1 (pt) 2021-08-17

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BR112013006594-0A BR112013006594B1 (pt) 2010-09-22 2011-09-20 Composto ciclopropano antagonista de receptor da orexina e composição farmacêutica

Country Status (28)

Country Link
US (1) US8268848B2 (ja)
EP (1) EP2626350B1 (ja)
JP (1) JP4944286B1 (ja)
KR (1) KR101458007B1 (ja)
CN (1) CN103153963B (ja)
AR (1) AR083060A1 (ja)
AU (1) AU2011304285B2 (ja)
BR (1) BR112013006594B1 (ja)
CA (1) CA2811895C (ja)
CL (1) CL2013000784A1 (ja)
DK (1) DK2626350T3 (ja)
ES (1) ES2540851T3 (ja)
IL (1) IL225437A (ja)
JO (1) JO2990B1 (ja)
MA (1) MA34609B1 (ja)
MX (1) MX2013003218A (ja)
MY (1) MY160969A (ja)
NZ (1) NZ609313A (ja)
PE (1) PE20131162A1 (ja)
PL (1) PL2626350T3 (ja)
PT (1) PT2626350E (ja)
RS (1) RS54101B1 (ja)
RU (1) RU2571414C2 (ja)
SG (1) SG188585A1 (ja)
SI (1) SI2626350T1 (ja)
TW (1) TWI516484B (ja)
UA (1) UA108510C2 (ja)
WO (1) WO2012039371A1 (ja)

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MX352881B (es) 2012-02-17 2017-12-13 Eisai R&D Man Co Ltd Metodos y compuestos utiles en la sintesis de antagonistas del receptor de orexina 2.
US9663513B2 (en) 2012-11-20 2017-05-30 Merck Sharp & Dohme Corp. Pyrimidine PDE10 inhibitors
MX366754B (es) * 2014-08-06 2019-07-23 Eisai R&D Man Co Ltd Método para producir compuesto de pirimidin-1-ol e intermedio de este.
CA2964504C (en) 2014-10-23 2022-08-23 Eisai R&D Management Co., Ltd. Oral dosage form comprising a cyclopropanecarboxamide derivative for use in treating insomnia
JP6885560B2 (ja) 2015-10-29 2021-06-16 国立大学法人 筑波大学 モルヒナン誘導体及びその医薬用途
RU2763493C2 (ru) 2016-05-12 2021-12-29 Эйсай Ар Энд Ди Менеджмент Ко., Лтд. Способы лечения расстройств циркадного ритма сна
JP7179049B2 (ja) * 2017-08-01 2022-11-28 ベルゲン ファーマシューティカル、 エルエルシー オレキシン受容体拮抗薬の結晶形及びその製造方法並びに用途
MX2021012833A (es) * 2019-05-15 2021-11-25 Eisai R&D Man Co Ltd Metodo y compuesto utiles en la preparacion del antagonista del receptor de orexina-2 y lemborexant que tiene pocas impurezas.
BR112021026291A2 (pt) * 2019-06-26 2022-03-03 Eisai R&D Man Co Ltd Lemborexant para tratar problemas de sono
US20240010629A1 (en) * 2019-12-11 2024-01-11 Teva Czech Industries S.R.O Solid state form of lemborexant
US20230051268A1 (en) 2019-12-20 2023-02-16 Eisai R&D Management Co., Ltd. Use of lemborexant for treating insomnia
JPWO2021145373A1 (ja) 2020-01-16 2021-07-22
WO2021205648A1 (ja) * 2020-04-10 2021-10-14 国立大学法人東海国立大学機構 精神障害患者の客観的睡眠評価方法
EP4376954A1 (en) 2021-07-26 2024-06-05 Eisai R&D Management Co., Ltd. Lemborexant for use in methods of treating irregular sleep-wake rhythm disorder and circadian rhythm sleep disorders associated with neurodegenerative diseases
WO2023178693A1 (zh) * 2022-03-25 2023-09-28 浙江华海药业股份有限公司 一种莱博雷生及其中间体的制备方法
WO2023178702A1 (zh) * 2022-03-25 2023-09-28 浙江华海药业股份有限公司 莱博雷生及其中间体化合物的制备方法

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US20120165339A1 (en) * 2010-12-22 2012-06-28 Eisai R&D Management Co., Ltd. Cyclopropane derivatives

Also Published As

Publication number Publication date
DK2626350T3 (en) 2015-06-29
IL225437A (en) 2015-05-31
CA2811895A1 (en) 2012-03-29
BR112013006594A2 (pt) 2016-06-21
MX2013003218A (es) 2013-06-28
TWI516484B (zh) 2016-01-11
AU2011304285B2 (en) 2015-01-29
EP2626350A1 (en) 2013-08-14
RU2571414C2 (ru) 2015-12-20
WO2012039371A1 (ja) 2012-03-29
PL2626350T3 (pl) 2015-08-31
AR083060A1 (es) 2013-01-30
CL2013000784A1 (es) 2013-07-05
CA2811895C (en) 2015-12-08
TW201305129A (zh) 2013-02-01
JPWO2012039371A1 (ja) 2014-02-03
ES2540851T3 (es) 2015-07-14
RU2013117464A (ru) 2014-10-27
UA108510C2 (en) 2015-05-12
PT2626350E (pt) 2015-08-03
AU2011304285A1 (en) 2013-05-16
EP2626350B1 (en) 2015-04-15
KR101458007B1 (ko) 2014-11-04
US20120095031A1 (en) 2012-04-19
KR20130097776A (ko) 2013-09-03
MA34609B1 (fr) 2013-10-02
NZ609313A (en) 2014-05-30
CN103153963A (zh) 2013-06-12
RS54101B1 (en) 2015-10-30
MY160969A (en) 2017-03-31
PE20131162A1 (es) 2013-10-19
SI2626350T1 (sl) 2015-09-30
IL225437A0 (en) 2013-06-27
SG188585A1 (en) 2013-04-30
US8268848B2 (en) 2012-09-18
JO2990B1 (ar) 2016-09-05
JP4944286B1 (ja) 2012-05-30
EP2626350A4 (en) 2014-02-12
CN103153963B (zh) 2014-12-24

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